| Stereochemistry | ABSOLUTE |
| Molecular Formula | C29H27N5O |
| Molecular Weight | 461.5576 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(=O)C(C2=CC=C3C=CC=CC3=C2)=C(N=C1NC[C@@H](N)CC4=CC=CC=C4)C5=CC=NC=C5
InChI
InChIKey=RQVKVJIRFKVPBF-VWLOTQADSA-N
InChI=1S/C29H27N5O/c1-34-28(35)26(24-12-11-21-9-5-6-10-23(21)18-24)27(22-13-15-31-16-14-22)33-29(34)32-19-25(30)17-20-7-3-2-4-8-20/h2-16,18,25H,17,19,30H2,1H3,(H,32,33)/t25-/m0/s1
AMG-548 is a selective and efficacious p38alpha inhibitor (Ki value is 0.5nM). Displays >1000-fold selectivity against 36 other kinases; inhibits whole blood LPS-stimulated TNFα (IC50 = 3 nM). Efficacious in acute and chronic models of arthritis. Clinical development of AMG-548 was terminated because of liver toxicity.
Originator
Approval Year
PubMed
Patents
ACTIVE MOIETY
